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Assay Detail

CHEMBL643074

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against human recombinant ATP-Citrate Lyase (ACL) enzyme
33
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

ATP-citrate synthase (CHEMBL3720)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.
Gribble AD, Ife RJ, Shaw A, McNair D, Novelli CE, Bakewell S, Shah VP, Dolle RE, Groot PH, Pearce N, Yates J, Tew D, Boyd H, Ashman S, Eggleston DS, Haltiwanger RC, Okafo G.
J Med Chem (1998) 41 : 3582 -3595
PubMed 9733484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 5.58 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120302 1 6.66
CHEMBL118107 3 6.52
CHEMBL122307 1 6.43
CHEMBL120008 1 6.26
CHEMBL120142 1 6.21
CHEMBL332774 1 6.15
CHEMBL332631 1 6.12
CHEMBL119628 2 6.11
CHEMBL119933 1 5.96
CHEMBL120906 1 5.75
CHEMBL324097 1 5.70
CHEMBL118966 1 5.57
CHEMBL263490 1 5.57
CHEMBL118726 1 5.54
CHEMBL121009 1 5.54
CHEMBL123646 1 5.50
CHEMBL330778 1 5.46
CHEMBL118407 1 5.41
CHEMBL116762 1 5.30
CHEMBL119643 1 5.29
CHEMBL116375 1 5.24
CHEMBL119937 1 5.02
CHEMBL120258 1 4.96
CHEMBL331772 1 4.89
CHEMBL325656 1 4.75
CHEMBL121651 1 4.72
CHEMBL118408 1 4.68
CHEMBL120393 1 4.39
CHEMBL120641 1 4.19
CHEMBL120253 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120302 Ki = 220.0 nM 6.66
CHEMBL118107 Ki = 300.0 nM 6.52
CHEMBL118107 Ki = 340.0 nM 6.47
CHEMBL122307 Ki = 370.0 nM 6.43
CHEMBL120008 Ki = 550.0 nM 6.26
CHEMBL118107 Ki = 580.0 nM 6.24
CHEMBL120142 Ki = 620.0 nM 6.21
CHEMBL332774 Ki = 710.0 nM 6.15
CHEMBL332631 Ki = 750.0 nM 6.12
CHEMBL119628 Ki = 770.0 nM 6.11
CHEMBL119628 Ki = 880.0 nM 6.06
CHEMBL119933 Ki = 1100.0 nM 5.96
CHEMBL120906 Ki = 1800.0 nM 5.75
CHEMBL324097 Ki = 2000.0 nM 5.70
CHEMBL263490 Ki = 2700.0 nM 5.57
CHEMBL118966 Ki = 2700.0 nM 5.57
CHEMBL118726 Ki = 2900.0 nM 5.54
CHEMBL121009 Ki = 2900.0 nM 5.54
CHEMBL123646 Ki = 3200.0 nM 5.50
CHEMBL330778 Ki = 3500.0 nM 5.46
CHEMBL118407 Ki = 3900.0 nM 5.41
CHEMBL116762 Ki = 5000.0 nM 5.30
CHEMBL119643 Ki = 5100.0 nM 5.29
CHEMBL116375 Ki = 5700.0 nM 5.24
CHEMBL119937 Ki = 9500.0 nM 5.02
CHEMBL120258 Ki = 11000.0 nM 4.96
CHEMBL331772 Ki = 13000.0 nM 4.89
CHEMBL325656 Ki = 18000.0 nM 4.75
CHEMBL121651 Ki = 19000.0 nM 4.72
CHEMBL118408 Ki = 21000.0 nM 4.68
CHEMBL120393 Ki = 41000.0 nM 4.39
CHEMBL120641 Ki = 64000.0 nM 4.19
CHEMBL120253 Ki = 160000.0 nM -